U0126-EtOH | MEK | AmBeed-信号通路专用抑制剂

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U0126-EtOH {[allProObj[0].p_purity_real_show]}

货号：A132258

U0126-EtOH（U0126）是一种高效、非ATP竞争性和选择性的MEK1和MEK2抑制剂，IC50值分别为72 nM和58 nM。它还抑制自噬和线粒体自噬。

U0126-EtOH 化学结构
CAS号：1173097-76-1

U0126-EtOH 3D分子结构
CAS号：1173097-76-1

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U0126-EtOH 纯度/质量文件产品仅供科研

货号：A132258 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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MEK 亚型比较

产品名称	MEK ↓ ↑	MEK1 ↓ ↑	MEK1/2 ↓ ↑	MEK2 ↓ ↑	MEK5 ↓ ↑	其他靶点	纯度
Honokiol	✔						98%
Mirdametinib	++++ MEK, IC50: 0.33 nM						99%+
Binimetinib	+++ MEK, IC50: 12 nM						99%+
BI-847325		++ MEK1, IC50: 25 nM		+++ MEK2, IC50: 4 nM			99%+
U0126-EtOH		+ MEK1, IC50: 0.07 μM		++ MEK2, IC50: 0.06 μM			98%
GDC-0623		++++ MEK1, IC50: 0.13 nM					99%+
TAK-733		++++ MEK1, IC50: 3.2 nM					99%+
Trametinib		++++ MEK1, IC50: 0.92 nM		++++ MEK2, IC50: 1.8 nM			99%+
Selumetinib		+++ MEK1, IC50: 14 nM MEK1, Kd: 99 nM		+ MEK2, Kd: 530 nM			99%+
CI-1040		++ MEK1, IC50: 17 nM		++ MEK2, IC50: 17 nM			99%+
Myricetin		✔					98%
Refametinib		++ MEK1, IC50: 19 nM		++ MEK2, IC50: 47 nM			99%+
Cobimetinib		+++ MEK1, IC50: 4.2 nM					99%+
PD98059		+ MEK1, IC50: 2 μM					99%+
SL327		+ MEK1, IC50: 0.18 μM		+ MEK2, IC50: 0.22 μM		AP-1	98+%
PD318088			✔				98%
AZD8330			+++ MEK1/2, IC50: 7 nM				99%+
Pimasertib							98%
(E/Z)-BIX02189					++++ MEK5, IC50: 1.5 nM		99%+
(E/Z)-BIX02188					+++ MEK5, IC50: 4.3 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

U0126-EtOH 生物活性

靶点	MEK2 MEK2, IC50:0.06 μM MEK1 MEK1, IC50:0.07 μM
描述	MEKs, which are members of the MAPKK family, can activate both ERK1 and ERK2 by catalyzing the phosphorylation on T202/Y204. Also MEK itself can be phosphorylated and activated through Ras when the upstream signaling is activated by extracellular stimuli, including growth factors, hormones etc.. U0126 is a selective MEK1/2 inhibitor with IC50 value of 70/60nM, but not ERK or Raf^[1]^[2]. Co-treatment with U0126 for 15min at concentration ranging in 1nM-10μM caused inhibition of PMA-induced p-ERK, the target of MEK1/2 in a dose-dependent manner in COS-7 cells. An in vitro study showed that U0126 represented much more potency to both wild type and ΔN3-S218E/S222D MEK compared with the another MEK1/2 inhibitor, PD98059^[2]. An in vivo study showed that U0126 is brain-permeable. Intravenous injection with U0126 at dose of 100mg/kg could reduce p-ERK1/2 in hippocampus after 10 min of reperfusion after 3.5 min bilateral carotid artery occlusion in male gerbils. Intravenous administration of U0126 at dose of 100-200mg/kg showed protective effect on the hippocampus against forebrain ischemia in male gerbils. Moreover, treatment with U0126 at 3 hours post ischemia significantly reduced volume after transient focal cerebral ischemia, accompanied with reduced p-ERK in the damaged brain areas^[3]. Also, it has been reported that U0126 helped maintain human pluripotent stem cells^[4].
作用机制	U0126 is a non-competitive inhibitor of MEK1/2, which can bind a common or two overlapping sites on MEK.^[2]

U0126-EtOH 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
COS-7 cells		Function assay		Inhibitory concentration against AP-1 transcription in COS-7 cells， IC50=1 μM.	15006386
HCT116 cells		Function assay		Ability of compound to inhibit anchorage independent colony formation (soft agar growth assay) in HCT116 cells, IC50=19.4 μM.	15225706
HeLa cells		Function assay		Inhibition of EGF-stimulated Elk1-luciferase reporter assay in HeLa cells, IC50=0.29 μM.	15225706
mouse RAS-3T3 cells	10-40 μM	Function assay		Inhibition of MEK-mediated ERK1/2 phosphorylation in mouse RAS-3T3 cells at 10 to 40 uM by ELISA.	24507826

U0126-EtOH 动物研究

Dose	Mice: 30 mg/kg^[7] (p.o.) Rat: 30 mg/kg^[8] (i.p.), 30 mg/kg^[9] (s.c.)
Administration	p.o., i.p., s.c.

U0126-EtOH 参考文献

[1]Duncia JV, Santella JB 3rd, et al. MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products. Bioorg Med Chem Lett. 1998 Oct 20;8(20):2839-44.

[2]Favata MF, Horiuchi KY, et al. Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J Biol Chem. 1998 Jul 17;273(29):18623-32.

[3]Namura S, Iihara K, et al. Intravenous administration of MEK inhibitor U0126 affords brain protection against forebrain ischemia and focal cerebral ischemia. Proc Natl Acad Sci U S A. 2001 Sep 25;98(20):11569-74. Epub 2001 Aug 14.

[4]Kinehara M, Kawamura S, et al. Protein kinase C regulates human pluripotent stem cell self-renewal. PLoS One. 2013;8(1):e54122.

[5]Duan W, Chan JH, et al. Anti-inflammatory effects of mitogen-activated protein kinase kinase inhibitor U0126 in an asthma mouse model. J Immunol. 2004;172(11):7053-9.

[6]Bokemeyer D, Panek D, et al. In vivo identification of the mitogen-activated protein kinase cascade as a central pathogenic pathway in experimental mesangioproliferative glomerulonephritis. J Am Soc Nephrol. 2002;13(6):1473-80.

U0126-EtOH 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.14mL

2.63mL

1.31mL

26.28mL

5.26mL

2.63mL

U0126-EtOH 技术信息

CAS号	1173097-76-1
分子式	C₂₀H₂₂N₆OS₂
分子量	426.558

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 50 mg/mL(117.22 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 2 mg/mL(4.69 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 35 mg/mL suspension

U0126-EtOH {[allProObj[0].p_purity_real_show]}

U0126-EtOH 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

U0126-EtOH 质控信息

U0126-EtOH 生物活性

U0126-EtOH 细胞研究

U0126-EtOH 动物研究

U0126-EtOH 参考文献

U0126-EtOH 实验方案

U0126-EtOH 技术信息

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U0126-EtOH {[allProObj[0].p_purity_real_show]}

U0126-EtOH 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

U0126-EtOH 质控信息

U0126-EtOH 生物活性

U0126-EtOH 细胞研究

U0126-EtOH 动物研究

U0126-EtOH 参考文献

U0126-EtOH 实验方案

U0126-EtOH 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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U0126-EtOH 纯度/质量文件产品仅供科研